Caduet 5/10

Caduet 5/10 is a medicinal product that belongs to a group of drugs that can have a direct effect on the heart and vascular system.

According to the ATC code, Caduet belongs to a combination of hypolipidemic agents, in particular, atorvastatin and amlodipine. The international name sounds like Atorvastatin and Amlodipine. Pharmacological group - HMG CoA reductase inhibitors.

Caduet 5/10 has proven its effectiveness and is widely used in cardiology practice. Due to its combined composition, the drug has a dual effect at the same time - it lowers blood pressure and reduces cholesterol levels, which is very convenient to use.

Indications Caduet 5/10

The drug is used in the presence of arterial hypertension, which has three or more risk factors for the development of concomitant cardiac and extracardiac pathology, for example, myocardial infarction, transient ischemic attack, stroke.

Indications for the use of Caduet 5/10 are the need for combined use of such drugs as hypocholesterolemic and antihypertensive drugs.

In addition, Caduet can be combined with other medications when cholesterol levels remain high and doses of antihypertensive drugs do not produce the desired result.

Indications for use of Caduet 5/10 are due to combined pathology, when the cholesterol level increases to such a level that atherosclerotic plaques begin to form. In turn, the latter reduce the internal diameter of the blood vessel.

As a result, there is a spasm of the vessels and an increase in intravascular resistance, which increases arterial pressure. As the number and volume of atherosclerotic plaques increase, there is an increasing load on the heart, since it must push blood through the vessels against high vascular resistance.

Release form

The tablet form of the drug allows you to control the dosage and avoid the occurrence of side effects if it is taken incorrectly.

The main active ingredients of the drug are amlodipine and atorvastatin. Each tablet contains 5 mg of amlodipine and 10 mg of atorvastatin. In addition, it should be noted that there are auxiliary components such as calcium carbonate, starch, colloidal anhydrous silicon dioxide, hydroxypropyl cellulose, magnesium stearate and many others.

The release form is a film-coated tablet. The main physical and chemical properties of the tablet preparation are white color, oval shape, film shell with the inscription "Pfizer" on the surface of one side and the drug code ("CDT" and "051") on the other.

The drug is packaged in 3 blisters in an outer cardboard box, each containing 10 tablets.

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Pharmacodynamics

The combined medicinal product is characterized by a dual mechanism of action, which determines the pharmacodynamics of Caduet 5/10.

It is necessary to consider separately the two active components of the drug. Thus, the action of amlodipine is based on its ability to affect muscle fibers by blocking slow calcium channels, being a representative of the group of calcium ion antagonists.

The amlodipine part of Caduet inhibits the flow of calcium ions through the membrane into the middle of the cells of smooth muscle fibers of blood vessels and the heart.

On the other hand, atorvastatin has an inhibitory effect on HMG-CoA reductase. It is a powerful selective inhibitor of this enzyme, the main task of which is considered to be the conversion of 3-hydroxy-3-methylglutaryl coenzyme A into melovate. The latter is a precursor of sterols, among which is cholesterol.

The pharmacodynamics of Caduet 5/10 determines the absence of modifications from both amlodipine and atorvastatin. The effect of amlodipine on blood pressure is noted to the same extent as when used as monotherapy. In turn, atorvastatin in Caduet also affects cholesterol levels, as when taken separately.

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Pharmacokinetics

Since the drug consists of two main components, the work of each should be considered separately. The pharmacokinetics of Caduet 5/10 is due to the action of amlodipine and atorvastatin.

After taking Caduet, absorption of amlodipine in a therapeutic dose ensures the peak plasma concentration in the interval from 6 to 12 hours after a single administration. Bioavailability is observed in the range of 64-80%. The distribution volume is about 21 l/kg. In addition, food intake does not affect the bioavailability of amlodipine.

In vitro studies have shown that in the body of a person suffering from hypertension, 97.5% of the drug circulates in the bloodstream in a complex with plasma proteins.

Approximately 90% of the administered dose of amlodipine is metabolized in the liver and converted into inactive metabolites. The elimination of the drug is a 2-stage process. About 10% of amlodipine and 60% of its metabolites are excreted in the urine. After a week of regular use of the drug, its level in the plasma is stable.

Pharmacokinetics of Caduet 5/10, considering atorvastatin, provides the first peak concentration already after 1-2 hours after a single dose of the drug. The degree of absorption directly depends on the dose of atorvastatin. The absolute level of bioavailability is approximately 12%, and the systemic one is 30%.

Low systemic bioavailability is due to the work of the digestive tract (stomach, intestines, liver). The absorption of the drug is affected by food intake, which slows it down.

However, despite this, the reduction in cholesterol occurs to the same extent, regardless of food intake and the time of use of the drug.

Approximately 95% of the drug is bound to plasma proteins and thus circulates in the bloodstream.

Elimination of atorvastatin and metabolites occurs primarily via bile after hepatic metabolism. Only 2% of the drug is excreted in urine.

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Dosing and administration

The medicine, due to its tablet form, is taken orally. At the beginning of the therapeutic course, the dose should not exceed 1 tablet per day.

The method of administration and dosage are determined depending on the stage of hypertension, the level of cholesterol in the blood and the presence of concomitant pathology.

If this dosage does not give the expected result (subject to daily intake of Caduet 5/10 for 7-10 days), then the dosage can be increased to 10 mg of amlodipine and 1 mg of atorvastatin.

The drug can be taken at any time of the day, regardless of food intake.

Caduet can be used in combination with other antihypertensive drugs, but with the exception of drugs that are calcium channel blockers.

As for lipid-lowering drugs, it is not recommended to use Caduet in parallel with an additional dosage of statins (drugs that reduce blood cholesterol levels).

Caduet should not be taken simultaneously with fibrates. In addition, the drug should be used with caution by people with liver and kidney pathology.

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Use Caduet 5/10 during pregnancy

During pregnancy, the woman's body requires strength and nutrients for the formation and development of the organs and systems of the fetus. Cholesterol and its derivatives are considered an important component of fetal growth.

Given the mechanism of action of atorvastatin, which consists of inhibiting HMG-CoA reductase and, accordingly, reducing cholesterol levels, there is a danger to the fetus.

Women who take Caduet for vital indications should use contraceptive protection. If a woman learns that she is pregnant, the drug should be discontinued.

The use of Caduet 5/10 during pregnancy is prohibited, since the benefit to the expectant mother does not outweigh the risk to the fetus.

In addition, there is no reliable data that amlodipine has the ability to penetrate into breast milk, however, based on evidence of atorvastatin penetration, the use of Caduet is therefore contraindicated during lactation.

Contraindications

It is necessary to highlight the main contraindications to the use of Caduet 5/10 in order to avoid the development of side effects and deterioration of health.

Contraindications include hypersensitivity to the group of dehydropyridine drugs, atorvastatin and amlodipine, as well as their excipients.

In addition, avoid taking the drug in case of severe liver pathology, elevated transaminase levels exceeding the upper limit by 3 or more times.

It is not recommended to take Caduet simultaneously with itraconazole, ketoconazole and telithromycin.

Contraindications to the use of Caduet 5/10 also include severe arterial hypertension, shock of various origins, aortic obstruction, unstable hemodynamics and the presence of unstable angina after myocardial infarction.

During the therapeutic course, it is necessary to monitor the level of liver enzymes and compare them with the baseline values that were recorded before starting to take Caduet.

The drug should be used with caution by people suffering from alcohol dependence, as well as those with a history of severe liver dysfunction.

Atorvastatin can affect skeletal muscles, causing pain syndrome, myositis and myopathy. Of course, throughout the therapeutic course, it is not worth monitoring the level of CPK, but in people with a tendency to acute necrosis of skeletal muscles and in the presence of muscle symptoms, it is still recommended to monitor the dynamics of CPK.

Side effects Caduet 5/10

Adverse events were assessed in 1092 patients undergoing treatment for hypertension and dyslipidemia compared with the placebo group.

Thus, the most frequent side effects of Caduet 5/10 were identified. Among the neurological symptoms, dizziness, drowsiness and headache in the occipital region should be highlighted. The digestive tract may react with dyspeptic disorders, nausea and abdominal pain. In addition, joint swelling, increased levels of liver enzymes and CPK were observed.

Rare side effects include allergic reactions, decreased sugar levels, weight gain, insomnia, depression, changes in skin sensitivity, and tinnitus.

Rare side effects of Caduet 5/10 include changes in the circulatory system in the form of a decrease in the level of leukocytes, platelets, vascular disorders - tachycardia, fainting, myocardial infarction and arrhythmia.

Very rarely, one can observe respiratory failure, mucous discharge from the nasal cavities, cough, vomiting, intestinal dysfunction with periodic constipation and diarrhea, as well as various disorders in the digestive and urinary systems.

Overdose

Cases of drug overdose are quite rare, since the drug is very easy to dose and, if taken as prescribed, is well tolerated by the body.

Overdosing on amlodipine can result in excessive dilation of blood vessels, which can result in a significant drop in blood pressure. Thus, hypotension of varying degrees will be observed for some time.

This condition definitely requires medical supervision and constant monitoring of the heart. In order to increase the pressure, you can use drugs that can narrow the blood vessels (vasoconstrictors).

However, they should be used with caution so as not to cause a sharp increase in blood pressure. In addition, amlodipine responds well to dialysis, which also reduces its concentration in the blood and reduces its therapeutic effect.

Overdose of atorvastatin is rare and has no specific antidote. Symptomatic treatment is necessary, including monitoring liver function, studying its enzymes and the level of CPK. Dialysis in this case will not lead to the expected result, since atorvastatin binds to blood proteins in small quantities.

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Interactions with other drugs

The simultaneous use of Caduet and certain medications can provoke the development of many side effects that negatively affect a person’s health.

Interaction of Caduet 5/10 with other drugs such as fibrates is not recommended, especially with gemfibrozil and infusion of dantrolene.

Since the drug contains atorvastatin, there is a risk, as with other representatives of the group of anticholesterolemic agents (statins), of developing acute muscle necrosis and myopathy.

This may occur when Caduet is used in combination with drugs that can increase plasma concentrations of atorvastatin. These include immunosuppressants (cyclosporine), macrolide antibiotics (erythromycin, clarithromycin), azole antifungals (itraconazole, ketoconazole, and nefazodone), lipid-modifying doses of niacin, gemfibrozil, and other fibric acid derivatives or HIV protease inhibitors.

In addition, the combined use of Caduet and fusidic acid is not recommended. If its use cannot be avoided, then during the therapeutic course of its use, atorvastatin should be discontinued.

In addition, amlodipine should be taken with caution simultaneously with baclofen, anticonvulsants - CYP3A4 inducers, alpha-1 blockers, amifostine, imipramine antidepressants, beta-blockers, hormonal drugs, other antihypertensive agents and sildenafil.

For atorvastatin, caution is required when co-administering it with cytochrome P450 3A4 inhibitors, protease inhibitors, warfarin, fusidic acid, niacin, antacids, grapefruit juice, hormonal contraceptives, colestipol, diltiazem, and phenazone.

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Storage conditions

Each medicine requires certain storage conditions. Thus, the storage conditions of Kaduet 5/10 must be met so that the drug does not lose its medicinal properties before the expiration date.

Storage conditions involve maintaining an optimal level of temperature, humidity and lighting in the room where the medication is planned to be stored for a long period of time.

Storage conditions for Kaduet 5/10 include temperatures not exceeding 30 degrees, as well as no exposure to direct sunlight to avoid premature loss of beneficial properties.

If certain conditions are not met, then the drug may change its structure, which in turn changes its pharmacokinetics and pharmacodynamics.

A mandatory condition for storing the drug is that it should not be accessible to children, as this may result in poisoning or the development of more serious consequences that threaten the lives of children.

Shelf life

When producing a medicine, the date of manufacture and last use of the drug must be indicated. This is the so-called expiration date.

It implies a certain period of time during which the drug retains its medicinal properties, but only if the storage rules are followed.

The shelf life of Caduet is 3 years. It is indicated on the outer cardboard packaging for quick access, as well as on each blister, so that if the packaging is lost, you know the date of the last dose.

Do not use the medicine after the expiration date.

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